Gras J
Barcelona, Spain.
Drugs Today (Barc). 2014 Nov;50(11):729-37. doi: 10.1358/dot.2014.50.11.2233783.
Acute bacterial skin and skin structure infections (ABSSSI) are associated with remarkable morbidity, and often require hospitalization. The cause of most ABSSSI is aerobic Gram-positive cocci, including Staphylococcus aureus, and β-hemolytic streptococci. Tedizolid phosphate is a novel oxazolidinone prodrug whose active moiety is tedizolid. It has shown potent in vitro activity against Gram-positive pathogens, encompassing methicillin-resistant S. aureus (MRSA) and strains resistant to vancomycin or linezolid. Animal studies suggested bactericidal activity in vivo. Pharmacokinetic studies demonstrated a good penetration into skin and soft tissues, and suitability for once-daily administration, either orally or intravenously at the same dosage. Pivotal phase III studies showed that tedizolid phosphate at 200 mg once daily for 6 days is noninferior to linezolid 600 mg twice daily for 10 days in ABSSSI patients, whereas gastrointestinal disorders were less frequent with tedizolid phosphate than linezolid. Tedizolid phosphate has been approved by the U.S. FDA, as Sivextro® to treat adult patients with ABSSSI.
急性细菌性皮肤及皮肤结构感染（ABSSSI）会引发显著的发病率，且常常需要住院治疗。大多数ABSSSI的病因是需氧革兰氏阳性球菌，包括金黄色葡萄球菌和β溶血性链球菌。磷酸特地唑胺是一种新型恶唑烷酮前药，其活性部分为特地唑胺。它在体外对革兰氏阳性病原体表现出强大的活性，包括耐甲氧西林金黄色葡萄球菌（MRSA）以及对万古霉素或利奈唑胺耐药的菌株。动物研究表明其在体内具有杀菌活性。药代动力学研究证明它对皮肤和软组织有良好的渗透性，并且适合每日一次给药，口服或静脉注射剂量相同。关键的III期研究表明，在ABSSSI患者中，每日一次服用200mg磷酸特地唑胺，持续6天，并不劣于每日两次服用600mg利奈唑胺，持续10天，而磷酸特地唑胺引起的胃肠道疾病比利奈唑胺更少。磷酸特地唑胺已被美国食品药品监督管理局批准，商品名为Sivextro®，用于治疗患有ABSSSI的成年患者。
